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Antagonism of histamine-activated adenylate cyclase in brain by D-lysergic acid diethylamide.

  • J. P. Green
  • , C. L. Johnson
  • , H. Weinstein
  • , S. Maayani

Research output: Contribution to journalArticlepeer-review

94 Scopus citations

Abstract

D-Lysergic acid diethylamide and D-2-bromolysergic acid diethylamide are competitive antagonists of the histamine activation of adenylate cyclase [ATP pyrophosphate-lyase (cyclizing); E.C. 4.6.1.1] in broken cell preparations of the hippocampus and cortex of guinea pig brain. The adenylate cyclase is linked to the histamine H2-receptor. Both D-lysergic acid diethylamide and D-2-bromolysergic acid diethylamide show topological congruency with potent H2-antagonists. D-2-Bromolysergic acid diethylamide is 10 times more potent as an H2-antagonist than cimetidine, which has been the most potent H2-antagonist reported, and D-lysergic acid diethylamide is about equipotent to cimetidine. Blockade of H2-receptors could contribute to the behavioral effects of D-2-bromolysergic acid diethylamide and D-lysergic acid diethylamide.

Original languageEnglish
Pages (from-to)5697-5701
Number of pages5
JournalProceedings of the National Academy of Sciences of the United States of America
Volume74
Issue number12
DOIs
StatePublished - Dec 1977

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